Глюкобай

General characteristics. Structure:

Active agent of 50 mg or 100 mg of acarbose. Excipients: silicon dioxide colloid anhydrous, magnesium stearate, starch corn, cellulose microcrystallic.
Description: Tablets of 50 mg: round biconvex tablets, white or white with a yellowish shade, with an engraving of branded marking (a bayerovsky cross) on one party and dosages of "G 50" on reverse.
Tablets of 100 mg - oblong biconvex tablets, white or white with a yellowish shade, with risky from two parties, on one of the parties the engraving designating a dosage - "G 100".

Pharmacological properties:

Pharmacodynamics. Active ingredient of the drug Glyukobay® - acarbose, is псевдотетрасахарид a microbic origin. Acarbose acts on digestive tract level, suppressing activity of enzymes of a small intestine (and - glucosidases) which participate in splitting of di - oligo-and polysaccharides. The dozozavisimy delay of digestion of carbohydrates with the subsequent slowed-down release and absorption of glucose which is formed in the course of splitting of carbohydrates results. Thus, acarbose detains and reduces postprandialny increase in concentration of glucose in blood. Owing to more balanced absorption of glucose from intestines, average concentration and its daily fluctuations in blood decrease. In case of increase in concentration of glikozilirovanny hemoglobin, acarbose reduces its level.
At patients with the broken tolerance to glucose (NTG *) regular purpose of acarbose leads to decrease in risk of development of a diabetes mellitus 2 types for 25%. Besides, it is established that at the same time at them the frequency of development of serdechnoksosudisty diseases (by 49%) and a myocardial infarction considerably decreases (for 91%).
Use of acarbose at a diabetes mellitus 2 types reduces risk of development of cardiovascular diseases by 24%, and a myocardium heart attack - for 64%.
* NTG is defined as blood plasma glucose level in 2 hours after meal in the range from 7.8 to 11.1 mmol/l (140-200 mg/dl) at glucose level on an empty stomach - from 5.6 to 7.0 mmol/l (100-1125 mg/dl).

Pharmacokinetics.

Absorption. About 35% of the entered dose are absorbed in the form of metabolites, less than 2% - in an active form. At least, 13 connections in the form of sulphatic, methyl and glucuronic conjugates are metabolized in digestive tract, mainly, by colibacilli and, only partially, digestive enzymes with education. One metabolite, a glucose molecule cleavage product in acarbose, has ability to inhibit alpha glucosidase. After reception of Glyukobaya® 2 peaks of the maximum concentration of acarbose in a blood plasma which average 52,2+ 15,7 mkg/l and 586,3+282,7 mkg/l are inside observed and are observed in 1,1+ 0,3 hours and 20,7+5,2 hours respectively. Emergence of the second peak is caused, apparently, by absorption of products of bacterial disintegration from deep departments of a small intestine. At patients with a renal failure (clearance of creatinine <25 ml/min. / 1.73 sq.m.) Stakh increases by 5 times, at elderly - by 1.5 times. Bioavailability makes 1-2%.

Distribution: the volume of distribution is 0,32 l/kg of body weight.

Removal: the elimination half-life for a phase of distribution and removal makes 3,7+2,7 hours and 9,6+4,4 hours respectively; 51% of active agent are removed through intestines; 1,7% in not changed look and in the form of an active metabolite and 34% in the form of metabolites - through kidneys.

Indications to use:

■ Treatment of a diabetes mellitus of type 2 in a complex with a dietotherapy (in the form of monotherapy or in a combination with other hypoglycemic drugs, including insulin)
■ Prevention of a diabetes mellitus of type 2 at patients with disturbance of tolerance to glucose in a combination with a diet and physical exercises.

Route of administration and doses:

The tablets Glyukobaya® are effective only if to accept them just before meal entirely, without chewing, with a small amount of liquid or chewing with the first portion of food.
The optimum dose of drug is selected the attending physician individually for each patient as its efficiency and portability vary.
Combination therapy in combination with a diet at patients with a diabetes mellitus 2 types
The initial dose makes 1 tablet on 50 mg 3 times a day or At a tablet on 100 mg 3 times a day. Further the dose should be raised to average daily-300 mg a day (2 tablets on 50 mg 3 times a day or 1 tablet on 100 mg 3 times a day).
In certain cases if necessary the dose of drug can be raised to 200 mg 3 times a day.

The dose should be raised with an interval of 4-8 weeks if at patients on the previous dose the necessary clinical effect is not gained.
If at the patient, despite strict observance of a diet, the meteorism and diarrhea amplify, then further increase in a dose of drug should be stopped, and in some cases and to reduce. The average daily dose of drug makes 300 mg a day.

Prevention of a diabetes mellitus 2 types at patients with disturbance of tolerance to glucose in a combination with a diet and physical exercises
The initial dose makes 50 mg once a day (tablets on 50 mg or At a tablet on 100 mg once a day). Within 3 months the initial dose gradually raises to the recommended therapeutic dose of 100 mg 3 times a day (2 tablets on 50 mg or 1 tablet on 100 mg 3 times a day)
Patients of advanced age (65 years are more senior): correction of a dose is not required. Children: use is contraindicated.
Liver failure: correction of a dose is not required.

Features of use:

Strict observance of an antidiabetic diet is obligatory at use of Glyukobaya®. Without consultation with the doctor it is impossible to cancel independently drug as drug withdrawal can be followed by increase in level of glucose in blood. In case of non-compliance with the diet ordered by the doctor side reactions from intestines can amplify. If symptoms amplify, despite strict observance of a diet, then it is necessary to consult with the doctor and to lower a drug dose for short or long term.
Глюкобай® possesses gipoklikemichesky action, but does not cause a hypoglycemia in patients to whom as therapy only observance of a diet without reception of glucose-lowering drugs is offered.
If Glyukobay® joins therapy by the insulin or drugs containing sulphonylurea or metformin, then, owing to decrease in need for these drugs, the hypoglycemia can develop, in rare instances up to a hypoglycemic coma that demands decrease in their dose. It must be kept in mind that Glyukobay® slows down transformation of sucrose into fructose and glucose therefore sucrose cannot be applied to stopping of an acute hypoglycemia. In these cases it is necessary to appoint glucose.
It is not recommended to combine Glyukobay® with Colestyraminum, intestinal adsorbents and drugs containing digestive enzymes. At the combined use with digoxin correction of a dose of the last can be required.

In the identification card which is available for the patient suffering from a diabetes mellitus the mark about treatment has to be made the drug Glyukobay®.
  правлять cars/mechanisms of Glyukobay does not render influence on ability.

Side effects:

Data on side effects of drug of Glyukobay are obtained from clinical trials and post-marketing messages.
The undesirable phenomena, are distributed on emergence frequency according to
following gradation: very often-> 10%, are frequent-> 1% <10%, infrequently-> 0,1% <1%, is rare-> 0,01% <0,1%.
The undesirable phenomena revealed during post-marketing monitoring are italicized.
From the blood circulatory system and lymphatic system: thrombocytopenia - the frequency of development is unknown;
From cardiovascular system: hypostases - it is rare;
From immune system: allergic reactions (rash, an erythema, a dieback, a small tortoiseshell) - the frequency of development is unknown;
From the alimentary system: a meteorism - it is very frequent, diarrhea, abdominal pains - it is frequent, nausea, vomiting, dyspepsia - it is rare, impassability or partial obstruction of intestines, a cystous pneumatosis intestinalis - the frequency of development is unknown.
From gepatobiliarny system:  passing increase in level of "hepatic" enzymes (including transaminases, an alkaline phosphatase and gamma transferase) - infrequently, jaundice - is rare, hepatitis - is very rare. Separate cases of fulminant hepatitis from the death took place in Japan. Their communication with acarbose is not clear.

Interaction with other medicines:

Sucrose and sakharozosoderzhashchy food at a combination to Glyukobayem® cause unpleasant feelings in a stomach up to diarrhea that is caused by the increased fermentation of carbohydrates in intestines. Colestyraminum, intestinal adsorbents and drugs containing digestive enzymes can exert impact on efficiency of Glyukobaya® at simultaneous use with it. In combination with dimetikonom/simetikony reactions of interaction are not observed. In certain cases Glyukobay® changes bioavailability of digoxin. Sulphonylurea derivatives, insulin, metformin strengthen hypoglycemic effect of acarbose. The drugs causing a hyperglycemia such as thiazide diuretics, glucocorticosteroids, фенотиазин, are oestrogenic, oral contraceptives, an isoniazid, niacin, Phenytoinum, adrenostimulyator, hormones of a thyroid gland, blockers of "slow" calcium channels, considerably reduce activity of acarbose (possibly development of a decompensation of a diabetes mellitus).

Contraindications:

■ Hypersensitivity to any component of drug
■ Age up to 18 years
■ the Chronic diseases of intestines proceeding with the expressed disturbances of digestion and absorption
■ States which are followed by a meteorism (Remkheld's syndrome, hernias of the big sizes, an intestinal stenosis, intestines ulcers)
■ Pregnancy and period of a lactation
■ Heavy renal failure (clearance of creatinine <25 ml/min.)

With care at fever, infectious diseases, injuries, surgical interventions. As at administration of drug perhaps asymptomatic increase in level of "hepatic" enzymes, within the first 6-12 months of treatment is recommended control of the level of these enzymes; usually at cancellation of Glyukobaya® their activity is normalized. Use at pregnancy and a lactation
As there are no data on use of Glyukobaya® during pregnancy and a lactation, it is not recommended to be applied at pregnant women and the feeding women.

Overdose:

If the high dose of Glyukobaya® is received together with the food and/or drinks containing carbohydrates (di - oligo-, polysaccharides), then the overdose can be followed by emergence of a meteorism and diarrhea. In case of overdose within the next 4-6 hours it is necessary to exclude the food or drinks containing carbohydrates from a diet. At reception of Glyukobaya® in the raised dose out of communication with meal development of symptoms from intestines is not supposed.

Storage conditions:

Period of validity 3 years. Not to use after expiry date. At a temperature not above 30 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 15 tablets in software the blister, on 2 or 8 blisters together with the application instruction in a cardboard pack Is scarlet/.